Assay Detail
Binding
CHEMBL683952
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards cloned human GluR7 subunit stably expressed in cultured HEK293 cells using [3]H-kainate as radioligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, kainate 3 (CHEMBL3684) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Pyrrolylquinoxalinediones carrying a piperazine residue represent highly potent and selective ligands to the homomeric kainate receptor GluR5.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 5.97 | 7.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL13076 | — | — | 1 | 7.34 |
| CHEMBL416685 | — | — | 1 | 6.28 |
| CHEMBL63861 | — | — | 1 | 6.17 |
| CHEMBL67828 | — | — | 1 | 5.85 |
| CHEMBL429540 | — | — | 1 | 5.85 |
| CHEMBL305534 | — | — | 1 | 5.60 |
| CHEMBL293613 | — | — | 1 | 5.39 |
| CHEMBL303415 | — | — | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL13076 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL416685 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL63861 | — | Ki | = | 680.0 | nM | 6.17 |
| CHEMBL67828 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL429540 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL305534 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL293613 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL303415 | — | Ki | = | 5700.0 | nM | 5.24 |